Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors

  • Bioorg Med Chem Lett. 1999 Nov 15;9(22):3187-92. doi: 10.1016/s0960-894x(99)00560-0.
C K Lau  1 ,  C Brideau ,  C C Chan ,  S Charleson ,  W A Cromlish ,  D Ethier ,  J Y Gauthier ,  R Gordon ,  J Guay ,  S Kargman ,  C S Li ,  P Prasit ,  D Riendeau ,  M Thérien ,  D M Visco ,  L Xu
Affiliations
  • 1. Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Québec, Canada.
PMID: 10576685 DOI: 10.1016/s0960-894x(99)00560-0
Abstract

A series of 3-heteroaryloxy4-phenyl-2-5H)-furanones were prepared and evaluated for their potency and selectivity as COX-2 inhibitors. This led to the identification of L-778,736 as a potent, orally active and selective inhibitor of the COX-2 enzyme.